Claims for Patent: 12,115,255

Summary for Patent: 12,115,255

Title:	Methods of use of emulsion formulations of an NK-1 receptor antagonist
Abstract:	Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.
Inventor(s):	Thomas B. Ottoboni, Han Han
Assignee:	Heron Therapeutics LLC
Application Number:	US18/418,030
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,115,255
Patent Claims:	1. An injectable emulsion, comprising: 0.7-0.8 wt % aprepitant; 13 wt/wt % to 20 wt/wt % of an emulsifier; an oil; a co-emulsifier which is an alcohol; a tonicity modifier; a pH modifier; and water; wherein the pH of the emulsion ranges from about 7.5 to 9.0. 2. The emulsion of claim 1, wherein the emulsifier is a phospholipid. 3. The emulsion of claim 2, wherein the phospholipid is present in the emulsion at about 17 wt/wt %. 4. The emulsion of claim 2, wherein the phospholipid is present in the emulsion at about 18 wt/wt %. 5. The emulsion of claim 1, wherein the emulsifier is an egg lecithin. 6. The emulsion of claim 5, wherein the egg lecithin is present in the emulsion at about 17 wt/wt %. 7. The emulsion of claim 5, wherein the egg lecithin is present in the emulsion at about 18 wt/wt %. 8. The emulsion of claim 5, wherein the ratio of egg lecithin to aprepitant is between about 20:1 to 25:1. 9. The emulsion of claim 5, wherein the ratio of egg lecithin to aprepitant is about 23:1. 10. The emulsion of claim 5, wherein the ratio of egg lecithin to aprepitant is about 24:1. 11. The emulsion of claim 5, wherein the ratio of egg lecithin to aprepitant is about 25:1. 12. The emulsion of claim 1, wherein the oil in the emulsion is soybean oil. 13. The emulsion of claim 12, wherein the soybean oil is present at a concentration of about 9 wt/wt % to 10 wt/wt %. 14. The emulsion of claim 1, wherein the alcohol in the emulsion is ethanol. 15. The emulsion of claim 14, wherein the ethanol is present in the emulsion at less than 10 wt/wt %. 16. The emulsion of claim 14, wherein the ethanol is present in the emulsion at a concentration of about 2 wt/wt % to 3 wt/wt %. 17. The emulsion of claim 1, wherein the tonicity modifier in the emulsion is sucrose. 18. The emulsion of claim 16, wherein the sucrose is present at a concentration of about 3 wt/wt % to 8 wt/wt %. 19. The emulsion of claim 16, wherein the sucrose is present at a concentration of about 5 wt/wt %. 20. The emulsion of claim 1, wherein the pH modifier in the emulsion is sodium oleate. 21. The emulsion of claim 19, wherein the sodium oleate is present at a concentration of about 0.4 wt/wt % to 0.5 wt/wt %. 22. The emulsion of claim 1, wherein the aprepitant is present in the emulsion at about 0.7 wt/wt %. 23. The emulsion of claim 21, wherein the phospholipid is an egg lecithin. 24. The emulsion of claim 21, wherein the ratio of phospholipid to aprepitant is between about 20:1 to 25:1. 25. The emulsion of claim 21, wherein the phospholipid is present at a concentration of about 17 wt/wt %. 26. The emulsion of claim 21, wherein the phospholipid is present at a concentration of about 18 wt/wt %. 27. The emulsion of claim 21, wherein the ratio of phospholipid to aprepitant is about 23:1. 28. The emulsion of claim 21, wherein the ratio of phospholipid to aprepitant is about 24:1. 29. The emulsion of claim 21, wherein the ratio of phospholipid to aprepitant is about 25:1. 30. An injectable pharmaceutical emulsion, comprising: about 0.7-0.8 wt % aprepitant; an egg phospholipid emulsifier; an oil; a co-surfactant; water; and a pH modifier, wherein the ratio of the emulsifier to aprepitant is about 20:1 to 25:1 (wt/wt %).